In 1893, P. Biginelli reported the synthesis of functionalized 3, 4-dihydropyrimidin-2(1H)-ones (DHPMs) via three-component condensation reaction of an aromatic aldehyde, urea, and ethyl acetoacetate. In the past decade, this long-neglected multicomponent reaction has experienced a remarkable revival, mainly due to the interesting pharmacological properties associated with this dihydropyrimidin...

Interactions of porphyrin derivatives 5,10,15,20-tetrakis(N-methylpyridinium-4-yl)-21H,23Hporphyrin (TMPyP4) and 5,10,15,20-tetrakis(N-propylpyridinium-4-yl)-21H,23H-porphyrin (TPrPyP4) with human telomeric AG3(T2AG3)3 G-quadruplex DNAs in 150 mM K -containing buffer in the presence or absence of 40% molecular crowding agent poly(ethylene glycol) (PEG 200) were studied by absorption titration f...

Different (±)-4-(3/4-acetoxyaryl)-5-ethoxycarbonyl-6-methyl-3,4-dihydropyrimidin-2-ones have been synthesized and subjected to enantioselective deacetylation reactions mediated by different lipases in organic media. Novozyme 435 in tetrahydrofuran:diisopropyl ether was found to be the catalyst of choice for efficient enantioselective deacetylation of dihydropyrimidinones under study. Further, w...

Introduction. Accumulation of middle molecular weight uremic toxins causes various complications in chronic hemodialysis (HD) patients. Postdilution online hemodiafiltration (OL-HDF) efficiently removes these molecules. This study aimed to assess the effectiveness three different dialysis membranes removing ?2- microglobulin (?2m) within a single session postdilution OL-HDF. Method. A prospecti...

A series of amino acid ester derivatives containing 5-fluorouracil were synthesized using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC*HCl) and N-hydroxybenzotriazole (HOBt) as a coupling agent. The structures of the products were assigned by NMR, MS, IR etc. The in vitro antitumor activity tests against leukaemia HL-60 and liver cancer BEL-7402 indicated that (R)-ethyl 2-(2...

A rapid and convenient synthesis of 5-unsubstituted 3,4-dihydropyrimidin-2-ones and thiones was developed. The reaction involves a one-pot reaction between oxalacetic acid, thiourea/urea, and aldehyde under microwave irradiation and provides the products in good yields and much shorter reaction times. 2010 Elsevier Ltd. All rights reserved.